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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Cerdulatinib
Cerdulatinib

Chemical Structure : Cerdulatinib

CAS No.: 1198300-79-6

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Cerdulatinib (PRT062070, PRT2070)

货号: PC-73204Not For Human Use, Lab Use Only.

Cerdulatinib (PRT062070) is a potent, ATP-competitive, orally active dual SYK/JAK inhibitor with IC50 of 32 nM (Syk), 0.5-12 nM (JAK1/2/3, Tyk2).

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10 mg ￥780 In stock
25 mg ￥1280 In stock
50 mg ￥2180 In stock
100 mg ￥3280 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Cerdulatinib (PRT062070) is a potent, ATP-competitive, orally active dual SYK/JAK inhibitor with IC50 of 32 nM (Syk), 0.5-12 nM (JAK1/2/3, Tyk2).
Cerdulatinib (PRT062070) has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma; Cerdulatinib (PRT062070) demonstrates specificity towards JAK1/JAK3 and TYK2, but not JAK2-mediated responses at cellular level, does not inhibit TCR signaling or PKC signaling in whole blood.
Cerdulatinib (PRT062070) blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E.
Cerdulatinib (PRT062070) induces cell cycle arrest and apoptosis under the condition of BCR stimulation in DLBCL cell lines.
Cerdulatinib (PRT062070) suppressed inflammation and autoantibody generation in a rat collagen-induced arthritis model and blocked B-cell activation and splenomegaly in a mouse model of chronic B-cell antigen receptor stimulation.

物理化学性质&存储条件

分子量 445.54
分子式 C20H27N7O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(Cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide

参考文献

1. Coffey G, et al. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.

2. Ma J, et al. Oncotarget. 2015 Dec 22;6(41):43881-96.

3. Blunt MD, et al. Clin Cancer Res. 2017 May 1;23(9):2313-2324.

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